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Target
Microtubule-associated protein tau
Ligand
BDBM610483
Substrate
n/a
Meas. Tech.
ChEMBL_2291542
IC50
120±n/a nM
Citation
 Hartz, RA; Ahuja, VT; Sivaprakasam, P; Xiao, H; Krause, CM; Clarke, WJ; Kish, K; Lewis, H; Szapiel, N; Ravirala, R; Mutalik, S; Nakmode, D; Shah, D; Burton, CR; Macor, JE; Dubowchik, GM Design, Structure-Activity Relationships, and In Vivo Evaluation of Potent and Brain-Penetrant Imidazo[1,2- J Med Chem 66:4231-4252 (2023) [PubMed] 
Target
Name:
Microtubule-associated protein tau
Synonyms:
MAPT | MAPTL | MTBT1 | Microtubule-associated protein tau | Neurofibrillary tangle protein | PHF-tau | Paired helical filament-tau | TAU | TAU_HUMAN | Tau Protein
Type:
Protein
Mol. Mass.:
78928.63
Organism:
Homo sapiens (Human)
Description:
P10636
Residue:
758
Sequence:
MAEPRQEFEVMEDHAGTYGLGDRKDQGGYTMHQDQEGDTDAGLKESPLQTPTEDGSEEPGSETSDAKSTPTAEDVTAPLVDEGAPGKQAAAQPHTEIPEGTTAEEAGIGDTPSLEDEAAGHVTQEPESGKVVQEGFLREPGPPGLSHQLMSGMPGAPLLPEGPREATRQPSGTGPEDTEGGRHAPELLKHQLLGDLHQEGPPLKGAGGKERPGSKEEVDEDRDVDESSPQDSPPSKASPAQDGRPPQTAAREATSIPGFPAEGAIPLPVDFLSKVSTEIPASEPDGPSVGRAKGQDAPLEFTFHVEITPNVQKEQAHSEEHLGRAAFPGAPGEGPEARGPSLGEDTKEADLPEPSEKQPAAAPRGKPVSRVPQLKARMVSKSKDGTGSDDKKAKTSTRSSAKTLKNRPCLSPKHPTPGSSDPLIQPSSPAVCPEPPSSPKYVSSVTSRTGSSGAKEMKLKGADGKTKIATPRGAAPPGQKGQANATRIPAKTPPAPKTPPSSGEPPKSGDRSGYSSPGSPGTPGSRSRTPSLPTPPTREPKKVAVVRTPPKSPSSAKSRLQTAPVPMPDLKNVKSKIGSTENLKHQPGGGKVQIINKKLDLSNVQSKCGSKDNIKHVPGGGSVQIVYKPVDLSKVTSKCGSLGNIHHKPGGGQVEVKSEKLDFKDRVQSKIGSLDNITHVPGGGNKKIETHKLTFRENAKAKTDHGAEIVYKSPVVSGDTSPRHLSNVSSTGSIDMVDSPQLATLADEVSASLAKQGL
  
Inhibitor
Name:
BDBM610483
Synonyms:
2-Cyclopropyl-N-(4-(4,4-difluoropiperidin-1-yl)pyridin-3-yl)imidazo[1,2-b]pyridazine-8-carboxamide | US10774086, Example 31
Type:
Small organic molecule
Emp. Form.:
C20H20F2N6O
Mol. Mass.:
398.4092
SMILES:
FC1(F)CCN(CC1)c1ccncc1NC(=O)c1ccnn2cc(nc12)C1CC1
Structure:
Search PDB for entries with ligand similarity: